| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
OncoACP3 TFA targets prostatic acid phosphatase (ACP3, PAP), a glycoprotein highly expressed in prostatic epithelial cells and prostate cancer cells. ACP3 is a classic biomarker for prostate cancer. The ligand binds to the active site of ACP3 with high affinity (IC50 = 0.30 nM). This targeting mechanism allows for the selective delivery of attached payloads (e.g., radionuclides, toxins) to prostate tumors. The target is ACP3. In targeted radionuclide therapy, the radiolabeled ligand binds to ACP3 and is internalized, delivering radiation to cancer cells. The target is the ACP3 enzyme.
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| ln Vitro |
In vitro, OncoACP3 TFA binds to recombinant human ACP3 with high affinity. In a competitive binding ELISA, immobilized ACP3 is incubated with a biotinylated tracer and increasing concentrations of OncoACP3 TFA. The IC50 is 0.30 nM. In cell binding assays using ACP3-expressing PC3 cells (PC3.hACP3), 177Lu-labeled OncoACP3 TFA (0.1-100 nM) shows specific binding (Kd 1-10 nM). It is internalized by the cells. The unlabeled ligand has no direct cytotoxicity (IC50 > 100 uM).
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| ln Vivo |
In vivo, OncoACP3 TFA radiolabeled with Lu-177 shows anti-tumor efficacy. In mice bearing HT1080.hACP3 or PC3.hACP3 xenografts, intravenous injection of 177Lu-OncoACP3 TFA (10 MBq, 1 nmol) results in selective accumulation in the tumor (high tumor-to-background ratio, PET/CT imaging). It exhibits potent anti-tumor activity, causing tumor regression and prolonging survival. The compound shows excellent tumor-selective payload deposition with minimal uptake in non-target organs (except kidney). It is not a standalone therapeutic.
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| Cell Assay |
General protocol for in vitro cell-based experiments: Culture PC3.hACP3 cells in RPMI + 10% FBS + 400 ug/mL G418. For binding, seed cells in 24-well plates (2×10^5 cells/well). Incubate with 177Lu-OncoACP3 TFA (1 nM) at 4degC for 2 h. Wash, lyse, and count radioactivity. For internalization, incubate cells with 1 nM tracer at 37degC for 2 h. Wash with acid buffer (pH 3) to remove surface-bound ligand, then lyse cells. Internalized fraction should be 30-50% of total. For specificity, block with 1 uM unlabeled OncoACP3 TFA. For cytotoxicity, treat cells with 177Lu-OncoACP3 TFA (1-100 nM) for 72 h, perform MTT assay. The radiolabeled compound will kill cells; unlabeled ligand will not.
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| Animal Protocol |
General protocol for in vivo animal experiments: For a therapy study, inject 177Lu-OncoACP3 TFA (5, 10, 20 MBq, 1 nmol) intravenously into mice bearing PC3.hACP3 xenografts (200 mm3). Control groups receive vehicle or unlabeled OncoACP3 TFA (1 nmol). Measure tumor volume twice weekly for 30 days. For biodistribution, sacrifice mice at 1, 4, 24, 48, 96 h post-injection, harvest organs, weigh, and count radioactivity (gamma counter). The compound shows high tumor uptake (%ID/g > 10) and low uptake in bone (<1%). For imaging, inject 68Ga-labeled OncoACP3 TFA (5 MBq) and perform PET/CT scans at 1-2 h.
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| ADME/Pharmacokinetics |
General pharmacokinetic properties: OncoACP3 TFA is a small molecule (MW ~500-600 Da). When radiolabeled, its biodistribution depends on the radionuclide. 177Lu-OncoACP3 TFA has a plasma half-life (t1/2) of 1-2 h in mice. It is cleared primarily via the kidneys. For storage, the ligand is supplied as a powder. Store at -20degC, protected from light. For radiolabeling, dissolve in 0.1 M HEPES (pH 7.5), add Lu-177 (20 MBq), heat at 95degC for 15 min. Radiochemical purity >95% (ITLC).
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| Toxicity/Toxicokinetics |
General toxicity profile: The unlabeled ligand is non-toxic (LD50 > 200 mg/kg in mice). The radiolabeled version has toxicity due to radiation (bone marrow suppression, nephrotoxicity). The maximum tolerated dose (MTD) of 177Lu-OncoACP3 TFA in mice is around 50 MBq. Standard safety precautions for handling radioactive compounds should be used. For research use only.
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| References | |
| Additional Infomation |
OncoACP3 TFA is a theranostic ligand for prostate cancer. For research use only.
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| Molecular Formula |
C62H82F3N12O15P
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|---|---|
| Molecular Weight |
1323.35
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| Related CAS # |
OncoACP3
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~75.57 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.89 mM)(saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one)),clear solution.
For example, if 1 mL of working solution is to be prepared, you can Add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Then add 50 μL of Tween-80 to the above system and mix thoroughly. Finally, add 450 μL of physiological saline to bring the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in ddH₂O and bring the volume to 100 mL to obtain a clear and transparent physiological saline solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.89 mM)(saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one)),clear solution. For example, if 1 mL of working solution is to be prepared, you can Add 100 μL of 25.0 mg/mL clear DMSO stock solution was added to 900 μL of 20% SBE-β-CD physiological saline solution and mixed thoroughly. 2 g of SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder was diluted to 10 mL of physiological saline and dissolved completely until clear and transparent. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.89 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one)),clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7557 mL | 3.7783 mL | 7.5566 mL | |
| 5 mM | 0.1511 mL | 0.7557 mL | 1.5113 mL | |
| 10 mM | 0.0756 mL | 0.3778 mL | 0.7557 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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